| Literature DB >> 21055954 |
Masato Yoshida1, Akira Mori, Atsuhiro Inaba, Masahiro Oka, Haruhiko Makino, Masashi Yamaguchi, Hisashi Fujita, Tomohiro Kawamoto, Mika Goto, Hiroyuki Kimura, Atsuo Baba, Tsuneo Yasuma.
Abstract
A series of novel tetrahydropyrazolopyrimidine derivatives containing an adamantyl group were synthesized and evaluated as potential calcium-sensing receptor (CaSR) antagonists. After chemical modification of 9a, which was identified as a hit compound in a random screening of CaSR antagonist assay, 7,7-dimethyl derivative 16c was found to be the most active compound of this new series (IC(50)=10nM). We report the synthesis of this series and their biological activities and structure-activity relationship.Entities:
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Year: 2010 PMID： 21055954 DOI： 10.1016/j.bmc.2010.10.035
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641